GSK1070916

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP02610CAS No. ：942918-07-2Purity：98%

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CAS No.	942918-07-2	Cat. No.	BCP02610
Name	GSK1070916
Synonyms	GSK 1070916;GSK-1070916;
SMILES
Chemical Name
Formula	C30H33N7O	M. Wt	507.63
Purity	98%	Storage	Store at 4-8°C
Description	GSK1070916 selectively inhibits Aurora B and Aurora C with Ki of 0.38 nM and 1.5 nM over Aurora A with Ki of 490 nM. Inhibition of Aurora B and Aurora C is time-dependent, with an enzyme-inhibitor dissociation half-life of >480 min and 270 min respectively. In addition, GSK1070916 is also a competitive inhibitor with respect to ATP. Human tumor cells treated with GSK1070916 shows dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific for Aurora B. Moreover, GSK1070916 inhibits the proliferation of tumor cells with EC50 values of <10 nM in over 100 cell lines spanning a broad range of tumor types, with a median EC50 of 8 nM. Although GSK1070916 has potent activity against proliferating cells, a dramatic shift in potency is observed in primary, nondividing, normal human vein endothelial cells. Furthermore, GSK1070916-treated cells do not arrest in mitosis but instead fails to divide and become polyploid, ultimately leading to apoptosis.In another st